Target intelligence / Profile preview

Proto-oncogene Mas (MAS1) (MAS1)

Target
MAS1
Molecular classification
G protein-coupled receptor, Receptor, Class A GPCR
01

Overview

The Mas G protein-coupled receptor (MAS1) is a critical component of the alternative renin-angiotensin system (RAS), specifically the ACE2/Ang-(1-7)/Mas axis [UniProt: P04201]. It primarily functions as the receptor for Angiotensin-(1-7), a peptide generated from Angiotensin II by the enzyme ACE2 [PubMed: 12815077]. Activation of the Mas receptor triggers signaling pathways that promote vasodilation, anti-fibrotic, anti-proliferative, and anti-inflammatory effects, effectively counteracting the deleterious actions of the classical Angiotensin II/AT1 receptor axis [PubMed: 23838351]. MAS1 is expressed in various tissues, including the heart, kidneys, and brain, where it plays a protective role against cardiovascular and renal injury [NCBI Gene: 4142]. In conditions like hypertension, heart failure, and diabetic nephropathy, the Mas receptor axis is often downregulated, contributing to disease progression [PubMed: 25164288]. Consequently, the Mas receptor is a significant therapeutic target, with synthetic agonists and Ang-(1-7) analogs being developed to restore the balance of the RAS and provide organ protection [PubMed: 29055815]. Its interaction with other receptors, such as the AT1 and bradykinin B2 receptors through heterodimerization, further modulates its physiological impact [PubMed: 16407465].

Other names
MAS1Mas-related G protein-coupled receptorMAS proto-oncogeneAngiotensin-(1-7) receptorMGPC
02

Mechanism of action

Activation of the Mas receptor by its primary ligand, Angiotensin-(1-7), triggers signaling pathways that counteract the vasoconstrictive and pro-inflammatory effects of the Angiotensin II/AT1 receptor axis [PubMed: 12815077].

03

Biological functions

Signal transductionVasodilationAnti-inflammatory responseAnti-fibrotic activityRegulation of blood pressureInhibition of cell proliferation
04

Disease associations

Cardiovascular diseaseHypertensionChronic kidney diseaseHeart failureInflammationDiabetesFibrosis
05

Safety considerations

HypotensionComplex receptor heterodimerization effects with AT1 and B2 receptorsLimited clinical data for synthetic agonistsPotential for off-target effects in the central nervous system
06

Interacting drugs

Angiotensin-(1-7)

6 more in the full profile.

07

Biomarkers

Angiotensin-(1-7) plasma levelsACE2 activity levelsACE2/ACE activity ratioUrinary Angiotensin-(1-7)

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